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Quinoline carboxamides for use in the treatment of leukemia

a technology of quinoline carboxamide and leukemia, which is applied in the field of quinoline carboxamide for use in the treatment of leukemia, can solve the problems of ineffectiveness, no benefit of roquinimex over placebo in relapse or survival, and no study on the effect of quinoline carboxamide roquinimex us

Active Publication Date: 2019-05-28
ACTIVE BIOTECH AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

Tasquinimod shows a surprisingly beneficial effect against leukemia, particularly acute leukemia, as demonstrated by its ability to reduce tumor burden and extend survival in murine xenograft models, offering a new therapeutic avenue for this disease.

Problems solved by technology

However, the study showed no benefit for Roquinimex over placebo regarding relapse or survival following ABMT for AML in remission.
Thus the quinoline carboxamide Roquinimex had been tested for use in the treatment of leukemia, but had been found ineffective.

Method used

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  • Quinoline carboxamides for use in the treatment of leukemia
  • Quinoline carboxamides for use in the treatment of leukemia
  • Quinoline carboxamides for use in the treatment of leukemia

Examples

Experimental program
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Effect test

example 1

[0134]Acute Myeloid Leukemia (AML)

[0135]U937 model—Ten million U937 cells (Monocytic human cell line, ATCC® CRL-1593.2TM) were injected i.v. in the tail vein of female C.B.-17 SCID mice. The mice were then randomly distributed into groups of 10-14 mice and received treatment with vehicle or tasquinimod ad lib in the drinking water. One group of mice was treated with tasquinimod 30 mg / kg / day and one group of mice was treated with vehicle, starting on the day of injection of U937 cells. The groups were terminated on day 21, before clinical signs of the tumor burden, and the tumor burden was analyzed in bone marrow by flow cytometry using a fluorochrome labeled anti-human CD45 antibody. The frequency of tumor cells found in bone marrow, in the tasquinimod treated group (n=14) and in the control group (n=1), respectively, is shown in FIG. 1.

example 2

[0136]Acute Lymphocytic Leukemia (ALL)

[0137]Tasquinimod was tested in a Patient Derived Xenograft (PDX) model AL-7015 provided by Crown Bioscience In. (www.crownbio.com). Cells derived from a patient with B-cell ALL were used. On Day 0, NOD / SCID mice were inoculated i.v. with 70×106 AL-7015-P2 leukemic cells per mouse. From day 1 to termination mice were treated with tasquinimod ad lib. in the drinking water at 30 mg / kg. Mice were terminated, as soon as any sign of morbidity was observed. The median survival time for the vehicle group was 51 days, while it was 99 days for the treatment group (p<0.0001) (FIG. 2). In the treatment group, the tumor burden remained close to zero for at least 10 weeks, long after the vehicle group had reached 100% tumor burden (FIG. 3).

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Abstract

A compound of formula (I) or a pharmaceutically acceptable salt thereof, for use in the treatment of leukemia.

Description

[0001]This application is a national phase of International Application No. PCT / EP2015 / 075769 filed Nov. 5, 2015 and published in the English language, and claims priority to EP 14193776.3 filed Nov. 19, 2014.FIELD OF THE INVENTION[0002]The present invention relates to certain quinoline carboxamides for use in the treatment of leukemia. More particularly, the invention relates to the compound 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethyl)phenyl]-1,2-dihydroquinoline-3-carboxamide (tasquinimod), or a pharmaceutically acceptable salt thereof, for use in the treatment of leukemia.BACKGROUND OF THE INVENTION[0003]Various therapeutically active quinoline carboxamides and a method for their preparation were described in International Applications No. PCT / SE99 / 00676, published as WO 99 / 55678 and No. PCT / SE99 / 01270, published as WO 00 / 03991, which applications disclosed the utility of these compounds for the treatment of diseases resulting from autoimmunity, such as multiple ...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K31/4704A61K9/20
CPCA61K9/20A61K31/4704A61P35/02A61K9/48
Inventor ERIKSSON, HELENASVENSSON, LEIFTORNGREN, MARIE
Owner ACTIVE BIOTECH AB